GSK525768A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK525768A 是 I-BET762 (GSK525762A) 的对映体、阴性对照化合物。

GSK525768A is an enantiomer, negative control compound of I-BET762 (GSK525762A), shows no activity against BET family proteins BRD2, BRD3 and BRD4.

GSK 525768A has no activity towards BET. GSK 525768A (GSK525768A) is the (R)-enantiomer of GSK525762A. GSK525762A is shown to regulate levels of the high-density lipid protein apolipoprotein A1 (APOA1) in assays monitoring APOA1 release in liver cells, whereas the (R)-enantiomer (GSK 525768A) has no effect. GSK 525768A directly engages the protein module by forming hydrogen bonds with the conserved asparagine residue in a way that mimics the binding mode of acetylated lysine; this usually results in the binding of the inhibitor deeper within the acetylated lysine binding site but without displacing the conserved water molecules that are present at the bottom of the acetyl-lysine binding cavity.

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GSK 525768A | GSK-525768A

Chromatin/Epigenetic

Bromodomain

Bromodomain

Inflammation/Immunology

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1260530-25-3

423.8954

C22H22ClN5O2

>98% (HPLC)

10 mM in DMSO

CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C

4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4R)-

(-20℃)

With Ice Pack

≥ 2 years